Фемостон®

General characteristics. Structure:

Active agent: oestradiol — 1 mg.

Excipients: lactoses monohydrate, gipromelloz, starch corn, silicon

dioxide colloid, magnesium stearate.

Cover dyes: Opadri OY-1-7000 white.

1 tablet of gray color contains:

Active agents: oestradiol — 1 mg, дидрогестерон — 10 mg.

Excipients: lactoses monohydrate, gipromelloz, starch corn, silicon

dioxide colloid, magnesium stearate.

Cover dyes: Opadri OY-8243 gray.

Description

Tablets of 1 mg of oestradiol:

Round biconvex tablets, coated, white color, with a stamping: on one party

tablets — "S" over a badge"

Pharmacological properties:

Pharmacological action - estrogen-gestagennoye.
Pharmacodynamics. Oestradiol — the estrogen which is a part of the drug Femoston® is identical to endogenous oestradiol of the person. Oestradiol fills shortage of estrogen in a female body after approach of a menopause and provides effective treatment of psychoemotional and vegetative climacteric symptoms: "inflows", the increased sweating, sleep disorders, the increased nervous irritability, dizziness, a headache, involution of skin and mucous membranes, especially mucous membranes of urinogenital system (dryness and irritation of a mucous membrane of a vagina, morbidity at the sexual intercourse). The Replacement Hormonal Therapy (RHT) the drug Femoston® prevents the loss of bone weight in the postmenopauzny period caused by deficit of estrogen. Administration of drug of Femoston® leads to change of a lipidic profile towards decrease in level of the general cholesterol and LPNP and increase in LPVP.

Didrogesteron represents progestogen, effective at intake which completely provides approach of a phase of secretion in an endometria, reducing thereby the risk of development of a hyperplasia of an endometria and/or carcinogenesis increasing against the background of estrogen. Didrogesteron has no oestrogenic, androgenic, anabolic or glucocorticosteroid activity.

The combination of 1 mg of oestradiol with didrogesterony represents the modern low-dosed ZGT mode.

Pharmacokinetics. After intake the micronized oestradiol easily is soaked up. It is metabolized in a liver to estrone and estrone of sulfate which is also exposed to hepatic biotransformation. Glucuronides of estrone and oestradiol are removed preferential with urine.

Didrogesteron after intake is quickly absorbed from a GIT. It is metabolized completely. The main metabolite — 20-digidrodidrogesteron, present at urine it is preferential in the form of a conjugate of glucuronic acid. Full removal of a didrogesteron happens in 72 h.

Indications to use:

ZGT at the frustration caused by the natural or come owing to surgical intervention menopause;

prevention of postmenopauzny osteoporosis.

Route of administration and doses:

Inside, it is desirable at the same time days, irrespective of meal — according to 1 tab. a day without interruption. ÖѼ«ßÔ«¡® 1/10 accept according to the following scheme: in the first 14 days of a 28-day cycle accept daily on 1 white tablet (from a half of packaging with the arrow marked with figure "1") containing 1 mg of oestradiol in the remained 14 days — daily on 1 gray tablet (from a half of packaging with the arrow marked with figure "2") containing 1 mg of oestradiol and 10 mg of a didrogesteron.

ÖѼ«ßÔ«¡® 2/10 accept according to the following scheme: in the first 14 days of a 28-day cycle accept daily 1 tab. of pink color (from a half of packaging with the arrow marked with figure "1") containing 2 mg of oestradiol, and in the remained 14 days — daily on 1 light yellow tablet (from a half of packaging with the arrow marked with figure "2") containing 2 mg of oestradiol and 10 mg of a didrogesteron.

Patients at whom periods did not stop are recommended to begin treatment in the first day of a menstrual cycle (the 1st day of the beginning of periods). With an irregular menstrual cycle it is reasonable to patients to begin treatment after 10–14 days of monotherapy by means of progestogen. Patients at whom the last periods were observed more than a 1 years ago can begin treatment at any time.

Features of use:

Before appointment or resuming of ZGT it is necessary to collect the full medical and family anamnesis and to conduct the general and gynecologic examination for the purpose of identification of the possible contraindications and states demanding observance of precautionary measures. During treatment drug recommends to inspect periodically women (frequency and character of researches are defined individually). Besides, it is reasonable to conduct a research of mammary glands and/or mammography according to accepted standards taking into account clinical indications. Use of estrogen can affect results of the following laboratory tests: definition of tolerance to glucose, a research of functions of a thyroid gland and liver.

The conventional risk factors of thromboses and thromboembolisms against the background of reception of ZGT are tromboembolic episodes in the anamnesis, severe forms of obesity (an index of body weight more than 30 kg/sq.m) and a system lupus erythematosus. Concerning a role of a varicosity in development of thromboembolisms there is no standard opinion.

The risk of development of a deep vein thrombosis of the lower extremities can temporarily increase at a long immobilization, extensive injuries or surgical interventions. When the long immobilization is necessary after surgical interventions, it is necessary to consider the possibility of the temporary termination of ZGT for 4–6 weeks before operation.

At the solution of a question of ZGT at the patients with a recurrent deep vein thrombosis or a thromboembolism receiving treatment by anticoagulants it is necessary to estimate advantage and risk of ZGT carefully.

If fibrinferments develop after the beginning of ZGT, drug should be cancelled. The patient should be informed on need of the address to the doctor in case of the following symptoms: painful puffiness of the lower extremities, sudden loss of consciousness, диспноэ, vision disorder.

There are data showing insignificant increase in frequency of identification of development of a breast cancer in women, is long (more than 10 years) the receiving ZGT. The probability of diagnosing of a breast cancer increases together with duration of treatment and is returned to norm in 5 years after the termination of ZGT.

The patients receiving earlier ZGT using only oestrogenic drugs have to be especially carefully inspected before an initiation of treatment for the purpose of identification of possible hyper stimulation of an endometria. Breakthrough uterine bleedings and unsharply expressed menstrualnopodobny bleedings can be noted in the first months of treatment by drug. If, despite correction of a dose, similar bleedings do not stop, drug has to be cancelled before establishment of the reason of bleeding. If bleeding recurs after the period of an amenorrhea or proceeds after treatment cancellation, it is necessary to establish its etiology. It can demand an endometria biopsy.

The drug Femoston® is not contraceptive. Patients in a perimenopauza are recommended to use non-hormonal contraceptives.

Influence on ability to driving and other mechanisms does not render.

Side effects:

Co of the party of blood and lymphatic system: very seldom (<0,01%) — hemolitic anemia.

From a nervous system: a headache, migraine (in 1–10%); sometimes (in 0,1–1%) — dizziness, nervousness, a depression, change of a libido; very seldom — a chorea.

From cardiovascular system: sometimes — a venous thromboembolism; very seldom — a myocardial infarction.

From a GIT: nausea, abdominal pains, meteorism; very seldom — vomiting.

From a liver and bilious ways: sometimes — cholecystitis; seldom (in 0,01–0,1%) — the abnormal liver function which sometimes is followed by an adynamy, an indisposition, jaundice or an abdominal pain.

From skin and hypodermic fatty tissue: sometimes — allergic reactions, rash, urticaria, an itch, peripheral hypostasis; very seldom — a hloazma, a melazma, a polymorphic erythema, a nodular erythema, a hemorrhagic purpura, a Quincke's disease.

From reproductive system and mammary glands: morbidity of mammary glands, breakthrough bleedings, pain in the field of a basin; sometimes — changes of an erosion of a neck of uterus, secretion change, a dysmenorrhea; seldom — increase in mammary glands, a predmenstrualnopodobny syndrome.

Others: changes of body weight; sometimes — vaginal candidiasis, a carcinoma of a mammary gland, increase in a leiomyoma in a size; seldom — intolerance of contact lenses, increase in curvature of a cornea; very seldom — a porphyria aggravation (<0,01%).

Interaction with other medicines:

The HP which are inductors of microsomal enzymes of a liver (barbiturates, Phenytoinum, rifampicin, рифабутин, carbamazepine), can weaken oestrogenic effect of the drug Femoston®. Ritonavir and нелфинавир, though are known as inhibitors of microsomal metabolism, can play a role of inductors at a concomitant use with steroid hormones. The drugs on the basis of herbs containing a St. John's Wort can stimulate exchange of estrogen and progestogens.

Interactions of a didrogesteron with other HP are unknown.

The patient should inform the doctor on medicines which she accepts now or accepted before purpose of the drug Femoston®.

Contraindications:

the established or alleged pregnancy;

breastfeeding period;

the diagnosed or suspected breast cancer, breast cancer in the anamnesis;

the diagnosed or suspected estrogenzavisimy malignant new growths;

vaginal bleedings of not clear etiology;

the idiopathic or confirmed thromboembolism of veins (deep vein thrombosis, thromboembolism of pulmonary vessels) previous;

the active or recently postponed arterial thromboembolism;

acute diseases of a liver, and also liver disease in the anamnesis (before normalization of laboratory indicators of function of a liver);

not treated hyperplasia of an endometria;

hypersensitivity to any of drug components;

porphyria.

With care — the patients who are coming into ZGT and having following fortune (now or in the past), have to be under fixed observation of the doctor:

uterus leiomyoma, endometriosis;

fibrinferments or their risk factors in the anamnesis;

risk factors of estrogenzavisimy tumors (for example a breast cancer at the patient's mother);

arterial hypertension;

benign tumor of a liver;

diabetes mellitus;

cholelithiasis;

epilepsy;

migraine or intensive headache;

endometria hyperplasia in the anamnesis;

system lupus erythematosus;

bronchial asthma;

renal failure;

otosclerosis.

After approval of the doctor administration of drug has to be stopped in such cases as:

emergence of jaundice or deterioration in function of a liver;

strong raising of the ABP;

for the first time the revealed migrenepodobny attack;

pregnancy;

manifestation of any contraindication.

Use at pregnancy and feeding by a breast

Contraindicated at pregnancy and during breastfeeding.

Overdose:

Symptoms: nausea, vomiting, drowsiness, dizziness.

Treatment: symptomatic.

Storage conditions:

At a temperature not above 30 °C. To store in the place, unavailable to children. Period of validity of the drug Фемостон® 3 of year.

Issue conditions:

According to the recipe

Packaging:

In the blister of 28 pieces (14 white and 14 gray); in a pack of cardboard 1, 3 or 10 blisters.
In the blister of 28 pieces (14 pink and 14 light yellow); in a pack of cardboard 1, 3 or 10 blisters.